リンシチニブ 化学特性,用途語,生産方法
効能
抗悪性腫瘍薬, インスリン様増殖因子受容体拮抗薬
説明
The binding of insulin-like growth factor 1 (IGF-1) to the IGF-1 receptor (IGF-1R) promotes cell growth while inhibiting apoptotic pathways. Overexpression of IGF-1R is found in certain solid tumors and hematologic neoplasias. However, insulin receptor (InsR) signaling can compensate for IGF-1R inhibition. Linsitinib is a dual inhibitor of IGF-1R and InsR kinases (IC
50s = 35 and 75 nM, respectively). It also inhibits InsR-
related receptor (IC
50 = 75 nM) but is without effect (IC
50 > 10 μM) against a large panel of other kinases. Linsitinib inhibits proliferation of a variety of tumor cell lines
in vitro and has antitumor efficacy in an IGF-1R-driven xenograft mouse model when administered orally. A rapid, non-invasive method to predict the pharmacodynamic response to linsitinib has been reported.
リンシチニブ 上流と下流の製品情報
原材料
準備製品